Chemical structures called cyclopropanes can enhance the effectiveness and customize the properties of many drugs, but traditional methods for creating this structure only work with specific molecules and require highly reactive—potentially explosive—ingredients.
Now, a team of researchers from Penn State has discovered and demonstrated a safe, efficient, and practical way to generate cyclopropanes on a wide range of molecules using a previously unknown chemical process. With further development, this new method—described in a paper published on August 4 in the journal Science—has the potential to revolutionize the drug development and production process.
Cyclopropanes are a crucial component in many drugs approved by the U.S. Food and Drug Administration, including those used to treat COVID-19, asthma, hepatitis C, and HIV/AIDS. These structures can enhance a drug’s potency, alter its solubility in the body, minimize unintended interactions, and fine-tune its performance. Cyclopropanes consist of a ring of three interconnected carbon atoms, with one carbon attached to the rest of the drug molecule and the other two each attached to two hydrogen atoms.
“Cyclopropanes are an essential part of many drugs, and incorporating them into drug candidates can be a significant aspect of the drug discovery process,” said Ramesh Giri, a chemistry professor in the Eberly College of Science at Penn State and leader of the research team.
“Previous attempts to improve the synthesis of cyclopropanes have focused on modifying a mechanistic pathway developed over 60 years ago. We approached this from a different perspective and identified an entirely new pathway that is simple, practical, and widely applicable.”
2023-08-03 14:48:02
Link from phys.org
